Nitrogen → N-(5-Bromo-2-chloro-3-pyridinyl)-4-(1-hydroxy-1-methylethyl)benzenesulfonamide

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Reaction Conditions

Reaction Steps

To a 100 mL, round-bottomed flask was added 4-acetyl-N-(5-bromo-2-chloropyridin-3-yl)benzenesulfonamide from Step 1 (250 mg, 642 μmol) and THF (10 mL). To this solution, methylmagnesium bromide (3.0 N, 4 mL, 12 mmol) was added in under N2 protection. The suspension was stirred at 25° C. for 3 h. The mixture was quenched by aqueous saturated NH4Cl. The aqueous part was extracted by 10% methanol-DCM (3×), and the combined organic was dried over MgSO4, and concentrated in vacuo to provide the title product as a yellow oil (250 mg), which was taken on to the next step without further purification. MS (ESI positive ion) m/z: 407 (M+1).

Provenance & Evidence